反应详情

A mixture of Example 10 step a (250 mg, 1.21 mmol), N-(2-bromoethyl)morpholine hydrochloride (306 mg, 1.32 mmol) and K2CO3 (500 mg, 3.62 mmol) in DMF (20 mL) was heated at 50° C. for 24 h. The reaction was then allowed to cool to RT and concentrated in vacuo. The residue was purified by FCC (DCM:MeOH, 1:0 to 9:1) to afford the title compound (479 mg, 98%) as a yellow oil. 1H NMR (300 MHz, CDCl3): δ 8.44 (1 H, dd, J 1.7, 1), 7.74-7.69 (1 H, m), 7.50 (1 H, t, J 7.9), 7.39-7.35 (2 H, m), 7.35-7.30 (1 H, m), 7.14-7.08 (1 H, m), 4.21 (2 H, t, J 5.6), 3.74 (4 H, t, J 4.6), 2.85 (2 H, t, J 5.6), 2.63-2.56 (4 H, m).

1. concentrationconcentrated in vacuo
2. customThe residue was purified by FCC (DCM:MeOH, 1:0 to 9:1)